Application of isodon henryi as Wnt signal path inhibitor and anti-cancer drug

A technology of carmin and signaling pathways, applied in the direction of antineoplastic drugs, drug combinations, active ingredients of esters, etc., to achieve clear pharmacological mechanisms, good medicinal value, and strong pharmacological effects

Active Publication Date: 2013-08-07
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the compound Exi caraway as a Wnt signaling pathway inhibitor in the prior art, and the application of the compound Exi caraway in the preparation of drugs for the prevention and treatment of colon cancer

Method used

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  • Application of isodon henryi as Wnt signal path inhibitor and anti-cancer drug
  • Application of isodon henryi as Wnt signal path inhibitor and anti-cancer drug
  • Application of isodon henryi as Wnt signal path inhibitor and anti-cancer drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Preparation of caraway from Hubei.

[0042] Dry leaves of Isodon rubescens var. lushanensis (Isodon rubescens var. lushanensis) 4Kg, pulverized, soaked in acetone / water solution at room temperature, combined extracts, distilled off the solvent under reduced pressure, suspended the crude extract in water, extracted with EtOAc, reduced pressure The solvent was recovered to obtain 117 g of extract. The extract was separated by silica gel column chromatography into 6 fractions: A-F. Fraction B (28g): 3 Fractions B were obtained by MCI column chromatography 1 -B 3 , where B 1 A mixture of two compounds was obtained by silica gel column chromatography (petroleum ether: acetone 1:0–0:1, gradient elution), and then separated by semi-preparative RP-18-HPLC (methanol: water, 30:70) to obtain the compound Hubei caraway (11.3mg).

[0043] Western Hubei henryin (see chemical structure figure 1 ) molecular formula is C 22 h 32 o 6 , molecular weight 392, white amorphous powd...

Embodiment 2

[0045] Exi caraway selectively inhibits colon cancer cell proliferation and induces colon cancer cell cycle arrest.

[0046] In the present invention, the MTS method is used to detect the anti-proliferation effect of the caramelin compound in western Hubei. After 72 hours of drug addition, compared with the broad-spectrum inhibitory effect of the cytotoxic chemotherapy drug cisplatin (cisplatin), Hubei caramelin showed a selective proliferation inhibitory effect on colon cancer cells (SW480, HCT116 The half-inhibitory concentration GI50 of the cells was 0.27 μM and 0.90 μM, respectively), and showed weak cytotoxicity to normal cells (human normal lung epithelial cells Beas-2B and human normal colonic epithelial cells CCD-841-CON) ( GI50 are 3.55μM and 2.98μM respectively) ( figure 2 A, 2B, 2C,). By analyzing the effect of Exi caraway on the cell cycle, it was found that with the prolongation of the treatment time of Hubei caraway (4 μM), more and more HCT116 colon cancer ce...

Embodiment 3

[0048] Exi caraway selectively inhibits Wnt signaling pathway in colon cancer cells.

[0049] In the present invention, firstly, the gene chip technology is used to detect the differential gene expression of the human colon cancer cells treated with the carrageenin in western Hubei. Hubei caraway (4μM) was incubated with SW480 for 12 hours, and the total RNA in SW480 cells was extracted for gene differential expression analysis. The results showed that a large number of genes in tumor-related signaling pathways were differentially expressed in SW480 cells treated with caraway in western Hubei. Through the analysis of differentially expressed genes, it was found that the expression of Wnt signaling pathway genes and their downstream target genes were significantly inhibited, and the analysis of signaling pathways proved that Wnt signaling pathway was the main affected signaling pathway ( image 3 A, 3B).

[0050] In most colon cancer cell lines, different gene mutations lead ...

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Abstract

The invention relates to an application of a small molecule compound isodon henryi as a Wnt signal path inhibitor and an application of isodon henryi in preparing a drug for preventing and treating a colon cancer. The isodon henryi disclosed by the invention is strong in pharmacological activity, clear in mode of action, safe and low-toxicity, good in stability, and can be used as a novel drug, a health-care product and / or a food additive, also can be used as a tool for researching the Wnt signal path.

Description

technical field [0001] The invention belongs to the field of medicaments, and in particular relates to the application of small molecule henryin in the fields of biotechnology and medicine. Background technique [0002] Colon tumor is a disease that seriously threatens human health and life. At present, there are three main methods of clinical treatment: surgery, radiotherapy and chemotherapy. Surgical treatment and radiotherapy are mainly aimed at local or regional tumors, and chemotherapy can only be relied on for tumors with multiple metastases throughout the body. Chemotherapy drugs currently used clinically are mostly cytotoxic drugs, which lack sufficient selectivity for colon cancer cells. While killing cancer cells, they also cause varying degrees of damage to normal tissue cells, resulting in therapeutic effects and patients' lives. Quality is affected. A large number of research results have shown that the excessive activation of the Wnt signaling pathway is clos...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P35/00A61K31/22
Inventor 李艳孙汉董普建新李兴尧张海波
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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